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Prolactin releasing effect of sulpiride isomers in rats and man

Journal Article:

Abstract

Sulpiride, an antipsychotropic drug of the benzamide class, reportedly displaces stereospecifically (/sup 3/H)-butyrophenones from putative dopamine (DA) binding sites in rat striatum. To evaluate if sulpiride displays the same stereospecifity in the inhibition of pituitary DA receptors, the effect of the two(-)-and (+)-sulpiride isomers was tested with regard to their ability to stimulate prolactin (PRL) secretion in rats and man and to displace (/sup 3/H)-spiroperidol bound to rat anterior pituitary receptors. In male rats, (-)-sulpiride at doses of 0.1 and 0.1 mg/kg i.p., induced a maximum PRL-releasing effect, not different from that evoked by a dose of 10 mg/kg of the compound. (+)-Sulpiride was active only at the dose of 10mg/kg i.p., and its PRL-releasing effect was superimposable to that evoked by the same dose of (-)-sulpiride. Similarily, in 8 normal subjects (4 men and 4 women) only (-)-sulpiride was active as PRL releaser when the low dose of 0.25 mg i.v. was used; when the higher dose of sulpiride was used (4.0 mg i.v.), it induced a rise in plasma PRL of the same entity for both isomers at early post-injection times (15-30 min) but greater with the (-)-isomer at the following time intervals (45-120 min). (-)-Sulpiride displaced (/sup  More>>
Authors:
Mueller, E E; Stefanini, E; Spano, P F; [1]  Camanni, F; Massara, F; [2]  Locatelli, V; Cocchi, D
  1. Cagliari Univ. (Italy). Inst. of Pharmacology and Pharmacognosy
  2. Turin Univ. (Italy). Chair of Endocrinology
Publication Date:
Jan 01, 1979
Product Type:
Journal Article
Reference Number:
AIX-11-565276; EDB-81-013136
Resource Relation:
Journal Name: J. Neural Transm.; (Austria); Journal Volume: 46:3
Subject:
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.; PITUITARY GLAND; STIMULATION; PSYCHOTROPIC DRUGS; BIOLOGICAL EFFECTS; DOPAMINE; ISOMERS; LTH; MAN; RADIOIMMUNOASSAY; RADIOPHARMACEUTICALS; RATS; RECEPTORS; TRITIUM; AMINES; ANIMALS; AROMATICS; BETA DECAY RADIOISOTOPES; BETA-MINUS DECAY RADIOISOTOPES; BODY; DRUGS; ENDOCRINE GLANDS; GLANDS; GONADOTROPINS; HORMONES; HYDROGEN ISOTOPES; HYDROXY COMPOUNDS; ISOTOPE APPLICATIONS; ISOTOPES; LABELLED COMPOUNDS; LIGHT NUCLEI; MAMMALS; MATERIALS; NUCLEI; ODD-EVEN NUCLEI; ORGANIC COMPOUNDS; ORGANS; PEPTIDE HORMONES; PHENOLS; PITUITARY HORMONES; POLYPHENOLS; PRIMATES; RADIOACTIVE MATERIALS; RADIOASSAY; RADIOISOTOPES; RODENTS; SYMPATHOMIMETICS; TRACER TECHNIQUES; VERTEBRATES; YEARS LIVING RADIOISOTOPES; 560305* - Chemicals Metabolism & Toxicology- Vertebrates- (-1987)
OSTI ID:
7028289
Country of Origin:
Austria
Language:
English
Other Identifying Numbers:
Journal ID: CODEN: JNTMA
Submitting Site:
INIS
Size:
Pages: 205-214
Announcement Date:

Journal Article:

Citation Formats

Mueller, E E, Stefanini, E, Spano, P F, Camanni, F, Massara, F, Locatelli, V, and Cocchi, D. Prolactin releasing effect of sulpiride isomers in rats and man. Austria: N. p., 1979. Web. doi:10.1007/BF01250786.
Mueller, E E, Stefanini, E, Spano, P F, Camanni, F, Massara, F, Locatelli, V, & Cocchi, D. Prolactin releasing effect of sulpiride isomers in rats and man. Austria. doi:10.1007/BF01250786.
Mueller, E E, Stefanini, E, Spano, P F, Camanni, F, Massara, F, Locatelli, V, and Cocchi, D. 1979. "Prolactin releasing effect of sulpiride isomers in rats and man." Austria. doi:10.1007/BF01250786. https://www.osti.gov/servlets/purl/10.1007/BF01250786.
@misc{etde_7028289,
title = {Prolactin releasing effect of sulpiride isomers in rats and man}
author = {Mueller, E E, Stefanini, E, Spano, P F, Camanni, F, Massara, F, Locatelli, V, and Cocchi, D}
abstractNote = {Sulpiride, an antipsychotropic drug of the benzamide class, reportedly displaces stereospecifically (/sup 3/H)-butyrophenones from putative dopamine (DA) binding sites in rat striatum. To evaluate if sulpiride displays the same stereospecifity in the inhibition of pituitary DA receptors, the effect of the two(-)-and (+)-sulpiride isomers was tested with regard to their ability to stimulate prolactin (PRL) secretion in rats and man and to displace (/sup 3/H)-spiroperidol bound to rat anterior pituitary receptors. In male rats, (-)-sulpiride at doses of 0.1 and 0.1 mg/kg i.p., induced a maximum PRL-releasing effect, not different from that evoked by a dose of 10 mg/kg of the compound. (+)-Sulpiride was active only at the dose of 10mg/kg i.p., and its PRL-releasing effect was superimposable to that evoked by the same dose of (-)-sulpiride. Similarily, in 8 normal subjects (4 men and 4 women) only (-)-sulpiride was active as PRL releaser when the low dose of 0.25 mg i.v. was used; when the higher dose of sulpiride was used (4.0 mg i.v.), it induced a rise in plasma PRL of the same entity for both isomers at early post-injection times (15-30 min) but greater with the (-)-isomer at the following time intervals (45-120 min). (-)-Sulpiride displaced (/sup 3/H)-spiroperidol bound to rat anterior pituitary homogenates with a potency about 100 times greater as that showed by (+)-sulpiride. In all, these data indicate that sulpiride isomers display at the level of pituitary DA receptors for PRL control the same stereospecifity exhibited on a population of striatal DA receptors.}
doi = {10.1007/BF01250786}
journal = {J. Neural Transm.; (Austria)}
volume = {46:3}
journal type = {AC}
place = {Austria}
year = {1979}
month = {Jan}
}